胃H，K - ATP酶的长效抑制剂。
Long lasting inhibitors of the gastric H,K-ATPase.
作者信息
Shin Jai Moo, Sachs George
机构信息
Department of Physiology, David Geffen School of Medicine, University of California at Los Angeles, and VA Greater Los Angeles Healthcare System, Los Angeles, CA 90073.
出版信息
Expert Rev Clin Pharmacol. 2009 Sep;2(5):461-468. doi: 10.1586/ecp.09.33.
Abstract
Proton pump inhibitors (PPIs) are acid-activated prodrugs which covalently bind to the gastric H,K-ATPase on its luminal surface. Only active pumps can be inhibited. The short plasma residence time of current PPIs prevents inhibition of pumps synthesized or activated after the PPI has disappeared, limiting the degree of acid inhibition even with BID administration. PPIs with a longer residence time should improve acid control. Various K(+) competitive inhibitors of the pump are being developed (APAs or PCABs), with the advantage of complete inhibition of acid secretion independent of pump activity. Early data on these suggest that twice a day administration would improve acid control compared to PPIs.
摘要
质子泵抑制剂（PPIs）是酸激活的前体药物，可与胃腔表面的胃H，K - ATP酶共价结合。只有活性泵才能被抑制。目前PPIs的血浆停留时间较短，这使得在PPI消失后合成或激活的泵无法被抑制，即使每日两次给药也限制了胃酸抑制程度。停留时间更长的PPIs应该能改善胃酸控制。目前正在研发各种钾离子竞争性泵抑制剂（APAs或PCABs），其优点是能完全抑制胃酸分泌，而与泵的活性无关。关于这些药物的早期数据表明，与PPIs相比，每日两次给药能改善胃酸控制。
相似文献
1
Long lasting inhibitors of the gastric H,K-ATPase.胃H，K - ATP酶的长效抑制剂。
Expert Rev Clin Pharmacol. 2009 Sep;2(5):461-468. doi: 10.1586/ecp.09.33.
2
The binding selectivity of vonoprazan (TAK-438) to the gastric H+, K+ -ATPase.沃克帕唑（TAK-438）对胃H⁺，K⁺ -ATP酶的结合选择性。
Aliment Pharmacol Ther. 2015 Dec;42(11-12):1315-26. doi: 10.1111/apt.13414. Epub 2015 Sep 30.
3
Revealing the Mechanistic Pathway of Acid Activation of Proton Pump Inhibitors To Inhibit the Gastric Proton Pump: A DFT Study.揭示质子泵抑制剂酸活化以抑制胃质子泵的作用机制途径：一项密度泛函理论研究
J Phys Chem B. 2016 Dec 29;120(51):13031-13038. doi: 10.1021/acs.jpcb.6b09334. Epub 2016 Dec 19.
4
Novel approaches to inhibition of gastric acid secretion.抑制胃酸分泌的新方法。
Curr Gastroenterol Rep. 2010 Dec;12(6):437-47. doi: 10.1007/s11894-010-0149-5.
5
Current status of acid pump antagonists (reversible PPIs).酸泵拮抗剂（可逆性质子泵抑制剂）的现状
Yale J Biol Med. 1996 May-Jun;69(3):233-43.
6
Pharmacokinetics and pharmacodynamics of the proton pump inhibitors.质子泵抑制剂的药代动力学和药效学。
J Neurogastroenterol Motil. 2013 Jan;19(1):25-35. doi: 10.5056/jnm.2013.19.1.25. Epub 2013 Jan 8.
7
Restoration of acid secretion following treatment with proton pump inhibitors.质子泵抑制剂治疗后胃酸分泌的恢复
Gastroenterology. 2002 Nov;123(5):1588-97. doi: 10.1053/gast.2002.36593.
8
Pharmacology of proton pump inhibitors.质子泵抑制剂的药理学
Curr Gastroenterol Rep. 2008 Dec;10(6):528-34. doi: 10.1007/s11894-008-0098-4.
9
Clinical pharmacology of proton pump inhibitors: what the practising physician needs to know.质子泵抑制剂的临床药理学：执业医师需要了解的内容。
Drugs. 2003;63(24):2739-54. doi: 10.2165/00003495-200363240-00004.
10
Improving on PPI-based therapy of GORD.优化基于质子泵抑制剂的胃食管反流病治疗方案。
Eur J Gastroenterol Hepatol. 2001 May;13 Suppl 1:S35-41.
引用本文的文献
1
Leveraging Omeprazole PBPK/PD Modeling to Inform Drug-Drug Interactions and Specific Recommendations for Pediatric Labeling.利用奥美拉唑药代动力学/药效学（PBPK/PD）模型来指导药物相互作用及儿科标签的具体建议。
Pharmaceutics. 2025 Mar 14;17(3):373. doi: 10.3390/pharmaceutics17030373.
2
In Vitro Metabolism and Transport Characteristics of Zastaprazan.扎斯塔拉唑的体外代谢和转运特性
Pharmaceutics. 2024 Jun 13;16(6):799. doi: 10.3390/pharmaceutics16060799.
3
RETRACTED: A Phase III Head-to-Head Study to Compare the Efficacy and Safety of Fexuprazan and Esomeprazole in Treating Patients with Erosive Esophagitis.撤回：一项比较非布司他和埃索美拉唑治疗糜烂性食管炎疗效和安全性的III期头对头研究。
J Clin Med. 2024 May 31;13(11):3262. doi: 10.3390/jcm13113262.
4
Association and Mechanisms of Proton Pump Inhibitors Use with Type-2Diabetes Mellitus Incidence in Adults: A Systemic Review andMeta-Analysis.质子泵抑制剂的使用与成年人 2 型糖尿病发病率的关联及其机制：系统评价和荟萃分析。
Curr Diabetes Rev. 2024;20(10):e120124225581. doi: 10.2174/0115733998254869231101095222.
5
Helicobacter Pylori: A Review of Current Treatment Options in Clinical Practice.幽门螺杆菌：临床实践中当前治疗选择的综述
Life (Basel). 2022 Dec 6;12(12):2038. doi: 10.3390/life12122038.
6
The role of vonoprazan in patients with erosive esophagitis.沃克帕唑在糜烂性食管炎患者中的作用。
Therap Adv Gastroenterol. 2022 Sep 13;15:17562848221122623. doi: 10.1177/17562848221122623. eCollection 2022.
7
Distribution- and Metabolism-Based Drug Discovery: A Potassium-Competitive Acid Blocker as a Proof of Concept.基于分布和代谢的药物发现：以钾竞争性酸阻滞剂为例的概念验证
Research (Wash D C). 2022 Jul 22;2022:9852518. doi: 10.34133/2022/9852518. eCollection 2022.
8
Will Proton Pump Inhibitors Increase the Risk of Diabetes Mellitus? A Systemic Review and Meta-Analysis.质子泵抑制剂会增加糖尿病的患病风险吗？一项系统性回顾和荟萃分析。
Turk J Gastroenterol. 2022 Jun;33(6):497-504. doi: 10.5152/tjg.2022.21480.
9
The Effect of Food on the Pharmacokinetics of the Potassium-Competitive Acid Blocker Vonoprazan.食物对钾离子竞争性酸阻滞剂沃诺拉赞药代动力学的影响。
Clin Pharmacol Drug Dev. 2022 Feb;11(2):278-284. doi: 10.1002/cpdd.1009. Epub 2021 Aug 24.
10
Evaluation of pharmacokinetic interactions between amoxicillin, clarithromycin, and the potassium-competitive acid blocker YH4808 in healthy subjects.健康受试者中阿莫西林、克拉霉素与钾竞争性酸阻滞剂YH4808之间的药代动力学相互作用评估。
Transl Clin Pharmacol. 2020 Mar;28(1):55-65. doi: 10.12793/tcp.2020.28.e5. Epub 2020 Mar 31.
本文引用的文献
1
Clinical trial: intragastric acid control in patients who have Barrett's oesophagus--comparison of once- and twice-daily regimens of esomeprazole and lansoprazole.临床试验：巴雷特食管患者的胃内酸度控制——埃索美拉唑和兰索拉唑一日一次和一日两次方案的比较。
Aliment Pharmacol Ther. 2009 Jul 1;30(2):138-45. doi: 10.1111/j.1365-2036.2009.04032.x. Epub 2009 Apr 29.
2
Review article: dual delayed release formulation of dexlansoprazole MR, a novel approach to overcome the limitations of conventional single release proton pump inhibitor therapy.综述文章：右兰索拉唑缓释胶囊的双重延迟释放制剂，一种克服传统单剂量质子泵抑制剂疗法局限性的新方法。
Aliment Pharmacol Ther. 2009 May 1;29(9):928-37. doi: 10.1111/j.1365-2036.2009.03984.x. Epub 2009 Feb 26.
3
Clinical trial: dexlansoprazole MR, a proton pump inhibitor with dual delayed-release technology, effectively controls symptoms and prevents relapse in patients with healed erosive oesophagitis.临床试验：双重迟释技术的质子泵抑制剂多潘立酮 MR 可有效控制症状并预防愈合的糜烂性食管炎患者复发。
Aliment Pharmacol Ther. 2009 Apr 1;29(7):742-54. doi: 10.1111/j.1365-2036.2009.03954.x. Epub 2009 Feb 7.
4
Failure of first-line eradication treatment significantly increases prevalence of antimicrobial-resistant Helicobacter pylori clinical isolates.一线根除治疗失败会显著增加耐抗菌药物幽门螺杆菌临床分离株的流行率。
J Clin Pathol. 2008 Oct;61(10):1112-5. doi: 10.1136/jcp.2008.060392. Epub 2008 Aug 28.
5
Predictable prolonged suppression of gastric acidity with a novel proton pump inhibitor, AGN 201904-Z.新型质子泵抑制剂AGN 201904-Z可实现可预测的胃酸分泌长期抑制。
Aliment Pharmacol Ther. 2008 Jul;28(2):187-99. doi: 10.1111/j.1365-2036.2008.03725.x. Epub 2008 Apr 25.
6
A randomized, comparative trial of a potassium-competitive acid blocker (AZD0865) and esomeprazole for the treatment of patients with nonerosive reflux disease.一项关于钾离子竞争性酸阻滞剂（AZD0865）与埃索美拉唑治疗非糜烂性反流病患者的随机对照试验。
Am J Gastroenterol. 2008 Jan;103(1):20-6. doi: 10.1111/j.1572-0241.2007.01544.x.
7
A randomized, comparative study of three doses of AZD0865 and esomeprazole for healing of reflux esophagitis.三种剂量的AZD0865与埃索美拉唑治疗反流性食管炎的随机对照研究
Clin Gastroenterol Hepatol. 2007 Dec;5(12):1385-91. doi: 10.1016/j.cgh.2007.08.014. Epub 2007 Oct 22.
8
Pharmacological profile of novel acid pump antagonist 7-(4-fluorobenzyloxy)-2,3-dimethyl-1-{[(1S,2S)-2-methyl cyclopropyl]methyl}-1H-pyrrolo[2,3-d]pyridazine (CS-526).新型酸泵拮抗剂7-(4-氟苄氧基)-2,3-二甲基-1-{[(1S,2S)-2-甲基环丙基]甲基}-1H-吡咯并[2,3-d]哒嗪（CS-526）的药理学特性
J Pharmacol Exp Ther. 2007 Oct;323(1):308-17. doi: 10.1124/jpet.107.121350. Epub 2007 Jul 13.
9
The gastric H,K ATPase as a drug target: past, present, and future.胃H⁺，K⁺-ATP酶作为药物靶点：过去、现在与未来。
J Clin Gastroenterol. 2007 Jul;41 Suppl 2(Suppl 2):S226-42. doi: 10.1097/MCG.0b013e31803233b7.
10
Soraprazan: setting new standards in inhibition of gastric acid secretion.索拉唑：在胃酸分泌抑制方面树立新标准。
J Pharmacol Exp Ther. 2007 Jun;321(3):866-74. doi: 10.1124/jpet.107.120428. Epub 2007 Mar 16.
Zotero 插件